Precursor-directed generation of indolocarbazoles with topoisomerase IIα inhibitory activity
© 2018 by the authors. One new indolocarbazole, 3-hydroxy-K252d (3), together with the recently reported 3-hydroxyholyrine A (1) and 3-N-acetyl-3-hydroxyholyrine A (2), were obtained by feeding a culture of the marine-derived Streptomyces strain OUCMDZ-3118 with 5-hydroxy-L-tryptophan. Their structu...
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| Main Authors: | , , , , , , |
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| Other Authors: | |
| Format: | Article |
| Published: |
2019
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| Subjects: | |
| Online Access: | https://repository.li.mahidol.ac.th/handle/123456789/47312 |
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| Institution: | Mahidol University |
| Summary: | © 2018 by the authors. One new indolocarbazole, 3-hydroxy-K252d (3), together with the recently reported 3-hydroxyholyrine A (1) and 3-N-acetyl-3-hydroxyholyrine A (2), were obtained by feeding a culture of the marine-derived Streptomyces strain OUCMDZ-3118 with 5-hydroxy-L-tryptophan. Their structures were elucidated on the basis of spectroscopic analysis. Compound 1 potently induced apoptosis of gastric cancer cells by inhibiting topoisomerase IIα enzyme activity and reducing the expression of antiapoptosis protein level. Compound 3 displayed moderate cytotoxicity against the A549 and MCF-7 cell lines with IC50 values of 1.2 ± 0.05 µM, 1.6 ± 0.09 µM, respectively. |
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